2. Apoptosis Membrane Transporter/Ion Channel
  3. Apoptosis GLUT
  4. GLUT4-IN-2

GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC50s of 11.4 µM and 6.8 µM for GLUT1 and GLUT4, respectively. GLUT4-IN-2 induces cell apoptosis and cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity.

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GLUT4-IN-2 Chemical Structure

GLUT4-IN-2 Chemical Structure

CAS No. : 2454113-83-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 165 In-stock
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10 mM * 1 mL in DMSO USD 165 In-stock
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5 mg USD 150 In-stock
10 mg USD 250 In-stock
25 mg USD 550 In-stock
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Based on 1 publication(s) in Google Scholar

GLUT4-IN-2 Related Antibodies

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Description

GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC50s of 11.4 µM and 6.8 µM for GLUT1 and GLUT4, respectively. GLUT4-IN-2 induces cell apoptosis and cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity[1].

IC50 & Target[1]

GLUT1

11.4 μM (IC50)

GLUT4

6.8 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
CCRF-CEM CC50
1.7 μM
Compound: F18
Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
[PMID: 32634629]
HS27 CC50
44 μM
Compound: F18
Cytotoxicity against human HS27 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
Cytotoxicity against human HS27 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
[PMID: 32634629]
K562 CC50
91.9 μM
Compound: F18
Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
[PMID: 32634629]
KCL-22 CC50
15.3 μM
Compound: F18
Cytotoxicity against human KCL-22 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
Cytotoxicity against human KCL-22 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
[PMID: 32634629]
MDA-MB-231 CC50
45.1 μM
Compound: F18
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
[PMID: 32634629]
In Vitro

GLUT4-IN-2 (compound F18) induces cell apoptosis and ell cycle arrest at G0/G1phase in CME cells[1].
GLUT4-IN-2 (10 µM; 6 h) decreases the expression of mTOR and CDK2, but increases the expression of GRP78, and cleaved caspase 3 proteins [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GLUT4-IN-2 Related Antibodies

Cell Viability Assay[1]

Cell Line: CME, K562, KCL-22, MB-231, HS-27 cells
Concentration: 1-100 µM
Incubation Time: 48 h
Result: Showed potent cytotoxicity with cytotoxic concentration 50% (CC50) of 1.7, 91.9, 15.3, 45.1, 44.0 µM for CME, K562, KCL-22, MB-231, HS-27 cells, respectively.

Apoptosis Analysis[1]

Cell Line: CEM cells
Concentration: 1.7 µM
Incubation Time: 24 h
Result: Induced cell apoptosis with the percentage of apoptotic cells in the late and early apoptosis region was 55.87% and 1.38%, respectively.

Cell Cycle Analysis[1]

Cell Line: CEM cells
Concentration: 10, 25, 50 µM
Incubation Time: 72 h
Result: Induced cell cycle arrest at G0/G1phase in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: CEM cells
Concentration: 10 µM
Incubation Time: 6 h
Result: Decreased the phosphorylation of mTOR and CDK2 proteins and increased the expression of GRP78, and cleaved caspase 3.

Cell Cytotoxicity Assay[1]

Cell Line: CEM cells
Concentration: 2.5-100 µM
Incubation Time: 48 h
Result: Showed cytotoxicity with the IC50s of 1.7, 187.2 µM for CEM, WBCs cells respectively.
In Vivo

GLUT4-IN-2 (50 mg/kg; i.p. on day 1–5, 8–12, 15–18) shows antitumor activity in CEM xenograft model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 8–10 weeks, SCID mice (CEM xenograft tumor) [1]
Dosage: 50 mg/kg
Administration: I.p.; administered on day 1-5, 8-12, 15-18
Result: Showed potent antitumor activity in vivo.
Molecular Weight

385.42

Formula

C17H11N3O4S2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NC1=NC2=CC=CC=C2S1)CN(C/3=O)C(SC3=C\C4=CC=CO4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (259.46 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5946 mL 12.9729 mL 25.9457 mL
5 mM 0.5189 mL 2.5946 mL 5.1891 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (6.49 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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(per animal)

μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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+
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5946 mL 12.9729 mL 25.9457 mL 64.8643 mL
5 mM 0.5189 mL 2.5946 mL 5.1891 mL 12.9729 mL
10 mM 0.2595 mL 1.2973 mL 2.5946 mL 6.4864 mL
15 mM 0.1730 mL 0.8649 mL 1.7297 mL 4.3243 mL
20 mM 0.1297 mL 0.6486 mL 1.2973 mL 3.2432 mL
25 mM 0.1038 mL 0.5189 mL 1.0378 mL 2.5946 mL
30 mM 0.0865 mL 0.4324 mL 0.8649 mL 2.1621 mL
40 mM 0.0649 mL 0.3243 mL 0.6486 mL 1.6216 mL
50 mM 0.0519 mL 0.2595 mL 0.5189 mL 1.2973 mL
60 mM 0.0432 mL 0.2162 mL 0.4324 mL 1.0811 mL
80 mM 0.0324 mL 0.1622 mL 0.3243 mL 0.8108 mL
100 mM 0.0259 mL 0.1297 mL 0.2595 mL 0.6486 mL
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GLUT4-IN-2 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GLUT4-IN-22454113-83-6ApoptosisGLUTGlucose transporterantitumorapoptosisCEM cellsG0/G1mTORCDK2GRP78cleaved caspase 3selectivecytotoxicityantiproliferativeInhibitorinhibitorinhibit

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